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ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS › ANTIPROTOZOALS › ANTIMALARIALS › Artemisinin and derivatives, combinations
artemisinin and piperaquine
P01BF07
Forms & Strengths
- Fixed-dose combination tablet: 20 mg artemisinin / 160 mg piperaquine
- Fixed-dose combination tablet: 40 mg artemisinin / 320 mg piperaquine
Adult Dosing
- Uncomplicated Plasmodium falciparum malaria: Total dose of 3 tablets per day (20/160 mg strength) or equivalent given once daily for 3 consecutive days
- Total target dose: artemisinin minimum 12 mg/kg and piperaquine minimum 54 mg/kg divided over 3 days
Pediatric Dosing
- Pediatric patients >6 months and >5 kg: Dosing based on body weight band
- Administered once daily for 3 consecutive days following weight-based national treatment guidelines
Indications
- Treatment of acute uncomplicated Plasmodium falciparum malaria
Mechanism of Action
- Artemisinin: Endoperoxide moiety undergoes iron-mediated cleavage generating free radicals that alkylate and damage parasite proteins
- Piperaquine: Bisquinoline compound that inhibits heme polymerization within the parasite digestive vacuole, leading to toxic heme accumulation
Contraindications
- Known hypersensitivity to artemisinin derivatives or piperaquine
- History of QT prolongation or congenital long QT syndrome
- Severe malaria
- Concomitant administration with drugs known to prolong the QT interval
Adverse Reactions
- Prolonged QT interval
- Headache
- Dizziness
- Anorexia
- Nausea and vomiting
- Abdominal pain
- Asthenia
Drug Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole) may increase piperaquine exposure and risk of QT prolongation
- Strong CYP3A4 inducers (e.g., rifampin) may decrease piperaquine efficacy
- Drugs prolonging the QT interval (e.g., antiarrhythmics, antipsychotics, macrolides) increase risk of fatal cardiac arrhythmias
Curated Content: Needs Vetting Before Put to Clinical Use